Biological Activity
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].
In Vitro
BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC50 of 110 nM. BPH-1358 against E. coli and S. aureus with EC50 of 300 nM and 290 nM, respectively[1].
In Vivo
BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)[1].
References & source
[1]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27.
[2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.